Caspase

Inhibitory Selectivity

Catalog No.	Inhibitor Name	Pan-Caspase	Caspase-1	Caspase-2	Caspase-3	Caspase-4	Caspase-5	Caspase-6	Caspase-7	Caspase-8	Caspase-9
A10984	VX-765 (Belnacasan)		**			***
A12373	Z-VAD-FMK	*
A13503	Z-DEVD-FMK
A14915	Q-VD-OPh hydrate		****		****					***	***
A14919	Caspase-3/7 Inhibitor I				****				***
A12611	Z-VEID-FMK
A12637	Z-VDVAD-FMK
A12697	Z-DQMD-FMK
A12800	Z-IETD-FMK
A14358	Z-LEHD-FMK
A14284	Z-FA-FMK
A15300	Ivachtin				****
A15392	Boc-D-FMK
A14916	Z-WEHD-FMK
A15816	Ac-DEVD-CHO		***	*	****	**	**	**	***	****	**

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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Boc-D-FMK

Catalog No. A15392
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Caspase 抑制剂

BOC-D-FMK是Caspase-3的新型抑制剂。了解更多

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Emricasan

Catalog No. A11394
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Caspase inhibitor

Emricasan is a first-in-class caspase inhibitor in clinical trials for the treatment of liver diseases. 了解更多

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Z-YVAD-FMK

Catalog No. A16317
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Caspase-1 抑制剂

Z-YVAD-FMK是有效的细胞渗透性和caspase-1不可逆抑制剂。了解更多

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Z-VAD(OH)-FMK

Catalog No. A16340
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Caspase 抑制剂

Z-VAD(OH)-FMK是所有胱天蛋白酶的不可逆三肽抑制剂。了解更多

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25-hydroxy Cholesterol

Catalog No. A13704
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25-hydroxy Cholesterol是一种衍生自膳食胆固醇的侧链取代氧固醇，可抑制固醇调节元件结合蛋白（SREBPs）的裂解，从而抑制各种细胞类型中的内源性胆固醇合成。了解更多

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Z-FA-FMK

Catalog No. A16381
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Cysteine protease 抑制剂

Z-FA-FMK是半胱氨酸蛋白酶的不可逆抑制剂。了解更多

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Z-FA-FMK

Catalog No. A14284
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Irreversible Cysteine Protease 抑制剂

Z-FA-FMK是不可逆的半胱氨酸蛋白酶抑制剂。了解更多

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MX1013

Catalog No. A17218
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pan-caspase inhibitor

MX1013 is a dipeptide pan-caspase inhibitor that inhibits caspase-1, caspase-3, and caspase-6, 7, 8, and 9. 了解更多

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LY573636 (Tasisulam)

Catalog No. A13070
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Apoptosis inducer

LY573636 (Tasisulam)是一种有效的抗肿瘤剂，在体外和体内引起多种人实体瘤的生长停滞和凋亡。LY573636诱导的凋亡通过线粒体靶向机制发生。了解更多

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- Ting TC, .et al. Aryl Sulfonamides Degrade RBM39 and RBM23 by Recruitment to CRL4-DCAF15, Cell Rep, 2019, Nov 5;29(6):1499-1510.e6 PMID: 31693891
- Ting Han, .et al. Anticancer sulfonamides target splicing by inducing RBM39 degradation via recruitment to DCAF15, Science, 2017, Apr 28;356(6336). pii: eaal3755 PMID: 28302793
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Apoptosis Activator 2

Catalog No. A11944
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Apoptosis Activator

Apoptosis Activator 2 强烈诱导caspase-3激活，PARP裂解和DNA片段化，导致细胞破坏（依赖Apaf-1），IC50为约4μM，对HMEC，PREC或MCF-10A细胞无效。了解更多

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PAC-1

Catalog No. A11090
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Caspase activator

PAC-1是procaspase-3的激活剂，可诱导癌细胞凋亡，EC50为2.08μM。了解更多

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- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
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EP1013

Catalog No. A11212
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caspase inhibitor

EP1013 is a broad-spectrum caspase selective inhibitor, used in the research of type 1 diabetes. 了解更多

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BOC-D-FMK

Catalog No. A11356
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caspase inhibitor

Boc-D-FMK is a cell-permeable, irreversible and broad spectrum caspase inhibitor; inhibits apoptosis stimulated by TNF-α with an IC50 of 39 ?M. 了解更多

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Z-IETD-FMK

Catalog No. A12800
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caspase 8 抑制剂

Z-IETD-FMK是caspase 8的特异性抑制剂。了解更多

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- Liqun Zhao, .et al. Rictor, an essential component of mTOR complex 2, undergoes caspase-mediated cleavage during apoptosis induced by multiple stimuli, Apoptosis, 2021, Apr 27 PMID: 33905036
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Z-DQMD-FMK

Catalog No. A12697
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Caspase-3 抑制剂

Z-DQMD-FMK是不可逆地抑制Caspase-3活性的合成肽。了解更多

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Z-VDVAD-FMK

Catalog No. A12637
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Caspase-2 抑制剂

Z-VDVAD-FMK是caspase-2的细胞渗透性不可逆抑制剂。半胱天冬酶抑制剂在研究生物学过程中起重要作用。了解更多

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Z-VEID-FMK

Catalog No. A12611
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Caspase-6 抑制剂

Z-VEID-FMK是caspase-6 / Mch2的特异性识别序列。 Z-VEID-FMK是不可逆地抑制VEID依赖性胱天蛋白酶（例如caspase-6）活性的合成肽。抑制剂被设计为甲酯，以促进细胞渗透性。了解更多

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Ac-DEVD-CHO

Catalog No. A15816
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Caspase 抑制剂

Ac-DEVD-CHO是醛肽和CPP32/Apopain抑制剂。了解更多

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ML132

Catalog No. A21557
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caspase 1 inhibitor

ML132 (NCGC 00185682) is a potent and selective caspase 1 inhibitor with an IC50 of 0.316 nM. 了解更多

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Ac-IEPD-AFC

Catalog No. A15319
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Fluorogenic caspase substrate

Ac-LEHD-AFC是caspase-4，caspase-5和caspase-9的荧光底物。了解更多

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PETCM

Catalog No. A15308
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Caspase-3 activator

PETCM是caspase-3的激活剂，也是HeLa细胞质中凋亡小体形成的刺激物。了解更多

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Ivachtin

Catalog No. A15300
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Caspase-3 抑制剂

Ivachtin是一种有效的，细胞可渗透的，可逆的，非竞争性的Caspase-3抑制剂（IC50 = 23 nM）。了解更多

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- Yosefzon Y, .et al. Caspase-3 Regulates YAP-Dependent Cell Proliferation and Organ Size, Mol Cell, 2018, May 17;70(4):573-587.e4 PMID: 29775577
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AZ 10417808

Catalog No. A15294
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Caspase-3 抑制剂

AZ 10417808，caspase-3的选择性非肽抑制剂（Ki = 247 nM）；相对于半胱氨酸蛋白酶1、2、6、7和8（Ki> 10 uM）显示的选择性> 40倍。了解更多

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Ac-LEHD-AFC

Catalog No. A15291
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Fluorogenic caspase substrate

Ac-LEHD-AFC，荧光半胱天冬酶底物。caspase-9底物的类似物LEHD-AFC。了解更多

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Caspase-3/7 Inhibitor I

Catalog No. A14919
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Caspase-3/7 抑制剂

Caspase-3/7 Inhibitor I是caspase-3（Ki = 60 nM）和caspase-7（Ki = 170 nM）的有效，细胞可渗透且可逆的有效抑制剂。了解更多

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Z-WEHD-FMK

Catalog No. A14916
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Caspase 抑制剂

Z-WEHD-FMK是不可逆抑制caspase-5和相关caspase活性的合成肽。了解更多

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Q-VD-OPh hydrate

Catalog No. A14915
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Caspase 抑制剂

Q-VD-OPh hydrate是一种选择性，脑和细胞可渗透的，高效且不可逆的caspase-3（IC50 = 25nm），caspase-1（IC50 = 50nM），caspase-8（IC50 = 100nM）和caspase-9抑制剂（IC50 ＝ 430nM）。了解更多

Product Citations (4)

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- Anna L Koessinger, .et al. Increased apoptotic sensitivity of glioblastoma enables therapeutic targeting by BH3-mimetics, Cell Death Differ, 2022, Apr 26 PMID: 35473984
- Florian J Bock, .et al. Apoptotic stress-induced FGF signalling promotes non-cell autonomous resistance to cell death, Nat Commun, 2021, Nov 12;12(1):6572 PMID: 34772930
- Davide Pradella, .et al. A ligand-insensitive UNC5B splicing isoform regulates angiogenesis by promoting apoptosis, Nat Commun, 2021, 12: 4872 PMID: 34381052
- Haschka MD, .et al. MARCH5-dependent degradation of MCL1/NOXA complexes defines susceptibility to antimitotic drug treatment, Cell Death Differ, 2020, Feb 3 PMID: 32015503
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Z-LEHD-FMK

Catalog No. A14358
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Caspase-9 抑制剂

Z-LEHD-FMK是一种不可逆抑制caspase-9和相关caspase活性的合成肽。了解更多

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- Wenquan Liang, .et al. Shikonin induces mitochondria-mediated apoptosis and enhances chemotherapeutic sensitivity of gastric cancer through reactive oxygen species, Sci Rep, 2016, 6: 38267 PMID: 27905569
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Z-DEVD-FMK

Catalog No. A13503
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Caspase-3 抑制剂

Z-DEVD-FMK是一种特殊的不可逆的Caspase-3抑制剂。了解更多

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- Roi Ankawa, .et al. Apoptotic cells represent a dynamic stem cell niche governing proliferation and tissue regeneration, Dev Cell, 2021, Jul 12;56(13):1900-1916 PMID: 34197726
- Yosefzon Y, .et al. Caspase-3 Regulates YAP-Dependent Cell Proliferation and Organ Size, Mol Cell, 2018, May 17;70(4):573-587.e4 PMID: 29775577
- Akashi E, .et al. Effects of galectin-9 on apoptosis, cell cycle and autophagy in human esophageal adenocarcinoma cells, Oncol Rep, 2017, Jul;38(1):506-514 PMID: 28586026
- Wenquan Liang, .et al. Shikonin induces mitochondria-mediated apoptosis and enhances chemotherapeutic sensitivity of gastric cancer through reactive oxygen species, Sci Rep, 2016, 6: 38267 PMID: 27905569
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Nivocasan (GS-9450)

Catalog No. A14100
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Caspase 抑制剂

Nivocasan (GS-9450)是一种新型的caspase抑制剂，已在纤维化/凋亡动物模型中证明了其肝保护活性。了解更多

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Z-VAD-FMK

Catalog No. A12373
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Pan Caspase 抑制剂

Z-VAD-FMK是一种细胞可渗透、不可逆的泛胱天蛋白酶抑制剂。体外抑制肿瘤细胞caspase加工和凋亡诱导(IC50 = 0.0015 - 5.8 mM)。活跃在体内。了解更多

Product Citations (30)

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- Ming-Chun Hung, .et al. AKT phosphorylation as a predictive biomarker for PI3K/mTOR dual inhibition-induced proteolytic cleavage of mTOR companion proteins in small cell lung cancer, Cell Biosci, 2022, 12: 122 PMID: 35918763
- Kaori Kanemaru, .et al. Plasma membrane phosphatidylinositol (4,5)-bisphosphate is critical for determination of epithelial characteristics, Nat Commun, 2022, May 9;13(1):2347 PMID: 35534464
- Chie Ishikawa, .et al. Exportin-1 is critical for cell proliferation and survival in adult T cell leukemia, Invest New Drugs, 2022, Aug;40(4):718-727 PMID: 35477814
- Aida Falgas, .et al. A diphtheria toxin-based nanoparticle achieves specific cytotoxic effect on CXCR4 + lymphoma cells without toxicity in immunocompromised and immunocompetent mice, Biomed Pharmacother, 2022, Jun;150:112940 PMID: 35421785
- Sumire Suzuki, .et al. Lysosome-targeted drug combination induces multiple organelle dysfunctions and non?canonical death in pancreatic cancer cells, Oncol Rep, 2022, Feb;47(2):40 PMID: 34958115
- Lina Y Abou Zeid, .et al. Caspase-mediated cleavage of miRNA processing proteins Drosha, DGCR8, Dicer, and TRBP2 in heat-shocked cells and its inhibition by HSP70 overexpression, Cell Stress Chaperones, 2022, Jan;27(1):11-25 PMID: 34719748
- Kosar Jabbari, .et al. Protein Ligands in the Secretome of CD36+ Fibroblasts Induce Growth Suppression in a Subset of Breast Cancer Cell Lines, Cancers (Basel), 2021, Sep 8;13(18):4521 PMID: 34572749
- Xiaoyue Deng, .et al. Setd1a Plays Pivotal Roles for the Survival and Proliferation of Retinal Progenitors via Histone Modifications of Uhrf1, Invest Ophthalmol Vis Sci, 2021, May 3;62(6):1 PMID: 33938913
- Liqun Zhao, .et al. Rictor, an essential component of mTOR complex 2, undergoes caspase-mediated cleavage during apoptosis induced by multiple stimuli, Apoptosis, 2021, Apr 27 PMID: 33905036
- Sofia Giacosa, .et al. Cooperative Blockade of CK2 and ATM Kinases Drives Apoptosis in VHL-Deficient Renal Carcinoma Cells through ROS Overproduction, Cancers (Basel), 2021, Feb 2;13(3):576 PMID: 33540838
- Hannes Schmid, .et al. Human invariant natural killer T cells promote tolerance by preferential apoptosis induction of conventional dendritic cells, Haematologica, 2021, Jan 14 PMID: 33440919
- Hua Xu, .et al. Preclinical Study Using ABT263 to Increase Enzalutamide Sensitivity to Suppress Prostate Cancer Progression Via Targeting BCL2/ROS/USP26 Axis Through Altering ARv7 Protein Degradation, Cancers (Basel), 2020, Apr; 12(4): 831 PMID: 32235588
- El-Ashmawy NE, .et al. Modulatory Effect of Silymarin on Apoptosis in Testosterone -Induced Benign Prostatic Hyperplasia in Rats, Pathol Oncol Res, 2020, Jan 4 PMID: 31902118
- Schneider D, .et al. The E3 ubiquitin ligase RNF40 suppresses apoptosis in colorectal cancer cells, Clin Epigenetics, 2019, Jul 2;11(1):98 PMID: 31266541
- Fujiki K, .et al. Blockade of ALK4/5 signaling suppresses cadmium- and erastin-induced cell death in renal proximal tubular epithelial cells via distinct signaling mechanisms, Cell Death Differ, 2019, Feb 25 PMID: 30804470
- T Yamamoto, .et al. Mycoplasma pneumoniae protects infected epithelial cells from hydrogen peroxide-induced cell detachment, Cell Microbiol, 2019, 2019 PMID: 30702185
- Maeda N, .et al. Glucocorticoids potentiate the inhibitory capacity of programmed cell death 1 by up-regulating its expression on T cells, J Biol Chem, 2019, Nov 13. pii: jbc.RA119.010379 PMID: 31723031
- Miyazawa S, .et al. Vitamin K2 induces non-apoptotic cell death along with autophagosome formation in breast cancer cell lines, Breast Cancer, 2019, Oct 17 PMID: 31625014
- Yeh HT, .et al. Flavopereirine induces cell cycle arrest and apoptosis via the AKT/p38 MAPK/ERK1/2 signaling pathway in human breast cancer cells, Eur J Pharmacol, 2019, Sep 10;863:172658 PMID: 31518562
- D. Bosc, .et al. A new quinoline-based chemical probe inhibits the autophagy-related cysteine protease ATG4B, Sci Rep, 2018, 8: 11653 PMID: 30076329
- Tsukamoto H, .et al. Lipopolysaccharide (LPS)-binding protein stimulates CD14-dependent Toll-like receptor 4 internalization and LPS-induced TBK1-IKKε-IRF3 axis activation, J Biol Chem, 2018, Jun 29;293(26):10186-10201 PMID: 29760187
- Hiroshi Kuribayashi, .et al. Roles of Nmnat1 in the survival of retinal progenitors through the regulation of pro-apoptotic gene expression via histone acetylation, Cell Death Dis, 2018, Sep; 9(9): 891 PMID: 30166529
- Matsuo J, .et al. Activation of caspase-3 during Chlamydia trachomatis-induced apoptosis at a late stage, Can J Microbiol, 2018, Oct 18:1-9 PMID: 30336068
- Orly Ravid, .et al. Blood-Brain Barrier Cellular Responses Toward Organophosphates: Natural Compensatory Processes and Exogenous Interventions to Rescue Barrier Properties, Front Cell Neurosci, 2018, 12: 359 PMID: 30459557
- Im E, .et al. Luteolin induces caspase-dependent apoptosis via inhibiting the AKT/osteopontin pathway in human hepatocellular carcinoma SK-Hep-1 cells, Life Sci, 2018, Sep 15;209:259-266 PMID: 30107166
- Szalai P, .et al. Nonlinear relationship between ER Ca2+ depletion versus induction of the unfolded protein response, autophagy inhibition, and cell death, Cell Calcium, 2018, Dec;76:48-61 PMID: 30261424
- Im E, .et al. Dihydroartemisinin induced caspase-dependent apoptosis through inhibiting the specificity protein 1 pathway in hepatocellular carcinoma SK-Hep-1 cells, Life Sci, 2018, Jan 1;192:286-292 PMID: 29128513
- Iriyama N, .et al. The cyclin-dependent kinase 4/6 inhibitor, abemaciclib, exerts dose-dependent cytostatic and cytocidal effects and induces autophagy in multiple myeloma cells, Leuk Lymphoma, 2018, Jun;59(6):1439-1450 PMID: 28918692
- Birte Plitzko, .et al. The natural product mensacarcin induces mitochondrial toxicity and apoptosis in melanoma cells, J Biol Chem, 2017, Dec 22; 292(51): 21102-21116 PMID: 29074620
- Akashi E, .et al. Effects of galectin-9 on apoptosis, cell cycle and autophagy in human esophageal adenocarcinoma cells, Oncol Rep, 2017, Jul;38(1):506-514 PMID: 28586026
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VX-765 (Belnacasan)

Catalog No. A10984
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Caspase-1/4 抑制剂

VX-765 (Belnacasan)是一种新型的Caspase-1抑制剂，是一种控制两种细胞因子IL-1b和IL-18生成的酶。了解更多

Product Citations (7)

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- Arjun Thapa, .et al. Danger-associated molecular pattern molecules take unexpectedly a central stage in Nlrp3 inflammasome-caspase-1-mediated trafficking of hematopoietic stem/progenitor cells, Leukemia, 2021, 23 February
- Prenitha Mercy Ignatius Arokia Doss, .et al. Male sex chromosomal complement exacerbates the pathogenicity of Th17 cells in a chronic model of central nervous system autoimmunity, Cell Rep, 2021, Mar 9;34(10):108833 PMID: 33691111
- Joseph Flores, .et al. Pre-symptomatic Caspase-1 inhibitor delays cognitive decline in a mouse model of Alzheimer disease and aging, Nat Commun, 2020, Sep 11;11(1):4571 PMID: 32917871
- Joseph Flores, .et al. Caspase-1 inhibition alleviates cognitive impairment and neuropathology in an Alzheimer's disease mouse model, Nat Commun, 2018, 9: 3916 PMID: 30254377
- Mohamed F. Ali, .et al. Canonical Stimulation of the NLRP3 Inflammasome by Fungal Antigens Links Innate and Adaptive B-Lymphocyte Responses by Modulating IL-1β and IgM Production, Front Immunol, 2017, 8: 1504 PMID: 29170665
- García-Fernández A, .et al. Targeting inflammasome by the inhibition of caspase-1 activity using capped mesoporous silica nanoparticles, J Control Release, 2017, Feb 28;248:60-70 PMID: 28069553
- Jiujiu Yu, .et al. Inflammasome activation leads to Caspase-1-dependent mitochondrial damage and block of mitophagy, Proc Natl Acad Sci U S A, 2014, 111(43): 15514-15519 PMID: 25313054